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Target
cAMP-dependent protein kinase catalytic subunit alpha [V123M,T183A]
Ligand
BDBM14027
Substrate
Kemptide
Meas. Tech.
Kinase Activity Assay
IC50
1350±n/a nM
Citation
 Bonn, S; Herrero, S; Breitenlechner, CB; Erlbruch, A; Lehmann, W; Engh, RA; Gassel, M; Bossemeyer, D Structural analysis of protein kinase A mutants with Rho-kinase inhibitor specificity. J Biol Chem 281:24818-30 (2006) [PubMed]  Article 
Target
Name:
cAMP-dependent protein kinase catalytic subunit alpha [V123M,T183A]
Synonyms:
KAPCA_BOVIN | PRKACA | cAMP-Dependent Protein Kinase (PKA) Mutant (V123M/T183A) | PKA C-alpha | cAMP-Dependent Protein Kinase (PKA) Mutant PKAR2 (3) | cAMP-dependent protein kinase, alpha-catalytic subunit
Type:
Enzyme Catalytic Subunit
Mol. Mass.:
40629.81
Organism:
Bovine
Description:
P00517[V123M,T183A]
Residue:
351
Sequence:
MGNAAAAKKGSEQESVKEFLAKAKEDFLKKWENPAQNTAHLDQFERIKTLGTGSFGRVMLVKHMETGNHYAMKILDKQKVVKLKQIEHTLNEKRILQAVNFPFLVKLEFSFKDNSNLYMVMEYMPGGEMFSHLRRIGRFSEPHARFYAAQIVLTFEYLHSLDLIYRDLKPENLLIDQQGYIQVADFGFAKRVKGRTWTLCGTPEYLAPEIILSKGYNKAVDWWALGVLIYEMAAGYPPFFADQPIQIYEKIVSGKVRFPSHFSSDLKDLLRNLLQVDLTKRFGNLKNGVNDIKNHKWFATTDWIAIYQRKVEAPFIPKFKGPGDTSNFDDYEEEEIRVSINEKCGKEFSEF
  
Inhibitor
Name:
BDBM14027
Synonyms:
AT877 | CHEMBL38380 | 5-(1,4-diazepan-1-ylsulfonyl)isoquinoline | 5-(1,4-diazepane-1-sulfonyl)isoquinoline | CHEMBL541388 | HA-1077 | cid_163751 | Fasudil (HA-1077) | US9687483, Fasudil | US20240246972, Compound Fasudil
Type:
Small organic molecule
Emp. Form.:
C14H17N3O2S
Mol. Mass.:
291.10
SMILES:
c1cc2cnccc2c(c1)S(=O)(=O)N3CCCNCC3
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Kemptide
Synonyms:
Aurora Peptide Substrate
Type:
Peptide
Mol. Mass.:
773.92
Organism:
n/a
Description:
50 uM ATP as co-substrate.
Residue:
7
Sequence:
LRRASLG